title: Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
abstract: A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxetine and atomoxetine (4 and 5).
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. ZhangP@wyeth.com
authors.forename: Puwen
authors.initials: P
authors.lastname: Zhang
authors.forename: Eugene A
authors.initials: EA
authors.lastname: Terefenko
authors.forename: Casey C
authors.initials: CC
authors.lastname: McComas
authors.forename: Paige E
authors.initials: PE
authors.lastname: Mahaney
authors.forename: An
authors.initials: A
authors.lastname: Vu
authors.forename: Eugene
authors.initials: E
authors.lastname: Trybulski
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Koury
authors.forename: Grace
authors.initials: G
authors.lastname: Johnston
authors.forename: Jenifer
authors.initials: J
authors.lastname: Bray
authors.forename: Darlene
authors.initials: D
authors.lastname: Deecher
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009638:Norepinephrine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism
chemical_list: D001562:Benzimidazoles; D014179:Neurotransmitter Uptake Inhibitors; D009638:Norepinephrine